LRRK2

NanoBRET Target Engagement Intracellular Kinase Assay, Competitive binding assay format

Target

LRRK2

HGNC Symbol

LRRK2

Synonyms

PARK8; ROCO2; FLJ45829

Cell Line

HEK293 human epithelial cell line from ATCC

Assay Format

384-well plate format using Promega’s NanoBRET TE Intracellular Kinase Assay

Assay Protocol

HEK293 cells transiently expressing NanoLuc- LRRK2 Fusion Vector were seeded into the wells of 384-well plates. The cells were pre-treated with the NanoBRET Tracer K-9 and then treated with reference compound CEP-701 for 1 hour. The BRET signal was measured on an Envision 2104 Multilabel Reader. IC50 value was calculated and IC50 curve was plotted using the GraphPad Prism 4 program based on a sigmoidal dose response equation.

Readout

Binding of compound to target kinase

Reference Compound IC50s
Compounds IC50 (M)
CEP-701 1.292e-008
Screening Location

Malvern, USA

Reference compound IC50 for LRRK2